2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. QNZ46

QNZ46 是一种高度选择性的非竞争性 NMDA 受体拮抗剂，靶向 GluN2C/D 亚基 (IC50=3.9 μM)，GluN1/GluN2C (IC50=7.1 μM) 和 GluN1/GluN2D (IC50=182 μM)。QNZ46 抑制谷氨酸介导的钙离子内流，从而阻断兴奋性毒性。QNZ46 具有膜渗透性，可通过血脑屏障，通过抑制髓鞘损伤和轴突退化。

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QNZ46 Chemical Structure

QNZ46 Chemical Structure

CAS No. : 1237744-13-6

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1 mg ￥228
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5 mg ￥600
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10 mg ￥1050
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QNZ46 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

QNZ46 is a highly selective noncompetitive NMDA receptor antagonist targeting GluN2C/D (IC50=3.9 μM), GluN1/GluN2C (IC50=7.1 μM), and GluN1/GluN2D (IC50=182 μM) subunits. QNZ46 inhibits glutamate-mediated calcium influx, thereby blocking excitotoxicity. QNZ46 is membrane permeable and can cross the blood-brain barrier, where it inhibits myelin damage and axonal degeneration[1][2][3].

IC50 & Target

NMDA Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Oocyte IC50
> 300 μM
Compound: 46
Antagonist activity at rat recombinant NR1-NR2B receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
Antagonist activity at rat recombinant NR1-NR2B receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
[PMID: 20684595]
Oocyte IC50
> 300 μM
Compound: 46
Antagonist activity at rat recombinant GLuR1 expressed in Xenopus oocytes assessed as inhibition of glutamate-induced current by two-electrode voltage-clamp electrophysiology
Antagonist activity at rat recombinant GLuR1 expressed in Xenopus oocytes assessed as inhibition of glutamate-induced current by two-electrode voltage-clamp electrophysiology
[PMID: 20684595]
Oocyte IC50
229 μM
Compound: 46
Antagonist activity at rat recombinant NR1-NR2A receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
Antagonist activity at rat recombinant NR1-NR2A receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
[PMID: 20684595]
Oocyte IC50
3 μM
Compound: 46
Antagonist activity at rat recombinant NR1-NR2D receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
Antagonist activity at rat recombinant NR1-NR2D receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
[PMID: 20684595]
Oocyte IC50
6 μM
Compound: 46
Antagonist activity at rat recombinant NR1-NR2C receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
Antagonist activity at rat recombinant NR1-NR2C receptor expressed in Xenopus oocytes at holding potential of -40mV by two-electrode voltage-clamp electrophysiology
[PMID: 20684595]
体外研究
(In Vitro)

细胞活力实验：QNZ46 (1-20 μM；48 h) 显著减少神经元细胞活力，抑制率与浓度正相关[2]。
免疫荧光实验：QNZ46 (50 μM；2 h) 减少髓鞘损伤模型中的髓鞘肿胀，保护结构完整性[2]。
WB 实验：QNZ46 (10 μM; 24 h) 抑制 MLKL 磷酸化和 RIP1 表达，可能对细胞坏死通路有抑制作用[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

QNZ46 相关抗体:

Cell Viability Assay[1]

Cell Line: HEK293 cells expressing GluN1/GluN2D receptors
Concentration: 1-20 μM
Incubation Time: 48 h
Result: Reduced cell viability by 23-88% (IC50=3.9 μM), consistent with noncompetitive NMDA receptor inhibition.

Immunofluorescence[2]

Cell Line: Primary oligodendrocytes
Concentration: 50 μM
Incubation Time: 24 h
Result: Reduced ischemic injury-induced myelin decompaction (G-ratio increase from 0.67 to 0.90 μm) and preserved FluoroMyelin Red staining intensity.

Western Blot Analysis[2]

Cell Line: Rat optic nerve (RON)
Concentration: 10 μM
Incubation Time: 24 h
Result: Decreased phosphorylated MLKL (30% reduction) and RIP1 expression (40% reduction), indicating suppression of necroptosis pathways[2].
体内研究
(In Vivo)

缺血性中风模型：QNZ46 (20 mg/kg；i.p.；单次给药) 显著减少暂时性大脑中动脉闭塞 (tMCAO) 小鼠脑损伤体积，改善神经功能[2]。
EAE 模型：QNZ46 (2 mg/kg+1 mg/kg CP465022；i.p.；每日 1 次，连续 28 天) 显著降低实验性自身免疫性脑脊髓炎 (EAE) 小鼠的临床评分，保护脊髓小直径髓鞘轴突[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (male, 25-30 g, 8-12 weeks) + transient middle cerebral artery occlusion (tMCAO)[2]
Dosage: 20 mg/kg (50% DMSO/β-cyclodextrin)
Administration: Single i.p. injection 120 min prior to ischemia
Result: Reduced infarct volume by 68%, preserved myelinated axons in the external capsule, and improved neurological performance.
Animal Model: Animal Model: . C57BL/6 mice (female, 20-22 g, 8-12 weeks) + experimental autoimmune encephalomyelitis (EAE)[3]
Dosage: 2 mg/kg QNZ46 + 1 mg/kg CP465022 (0.5% methyl cellulose)
Administration: Daily i.p. injections from day 0 to day 28 post-immunization
Result: Combined QNZ46/CP465022 treatment reduced clinical severity and preserved small-diameter myelinated axons in spinal cord.
分子量

443.41

Formula

C24H17N3O6
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4 mg/mL (9.02 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2552 mL 11.2762 mL 22.5525 mL
5 mM 0.4510 mL 2.2552 mL 4.5105 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

QNZ46 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2552 mL 11.2762 mL 22.5525 mL 56.3812 mL
5 mM 0.4510 mL 2.2552 mL 4.5105 mL 11.2762 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

QNZ461237744-13-6QNZ 46QNZ-46iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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